SB743921 |
| Catalog No.GC14600 |
SB743921 is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 940929-33-9
Sample solution is provided at 25 µL, 10mM.
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SB743921 is an inhibitor of kinesin spindle protein (KSP) with Ki value of 0.1nM [1].
As an inhibitor of mitotic kinesin KSP, SB743921 causes cell cycle arrest in mitosis, results in cell death. SB743921 is developed to treat for cancers. SB743921 is a potent and selective inhibitor. In the affinity assays, SB743921 shows Ki values of 0.1nM and 0.12nM for human KSP and mouse KSP, respectively. It has no affinity with other kinesins. In the cellular assay, SB743921 exerts anti-proliferation efficacy in SKOV3, Colo205, MV522 and MX1 with IC50 values of 0.02nM, 0.07nM, 1.7nM and 0.06nM. Moreover, SB743921 is shown to have activity against human tumor xenografts Colo205, MCF-7, SK-MES, H69, OVCAR-3, HT-29, MDA-MB-231 and A2780. SB743921 is also effective against P388 lymphocytic leukemia xenografts in mice [1].
References:
[1] Jackson J R, Gilmartin A, Dhanak D, et al. A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer. Proceedings of the American Association for Cancer Research, 2006, 2006(2): B11.
Cell experiment: | K562 and KCL22 cells are seeded in six-well plates at a number of 5 × 105 in 2 mL RPMI-1640 medium supplemented with 10% FBS in a 5% CO2 atmosphere at 37°C, and are treated with control (2% DMSO), 50 nM imatinib, 2 nM SB-743921 and 50 nM imatinib + 2 nM SB-743921, respectively. Cell number and viability are determined every 24 h. Results are plotted for live cells against time to generate a growth curve[2]. |
Animal experiment: | The animal experiments are performed with female NMRI nu/nu mice. Tumor fragments are obtained from xenografts in serial passage in nude mice. Mice are randomized to the various groups, and dosing is started when the required number of mice carries a tumor of 50-250 mm3 volume, preferably 80-200 mm3. Vehicle for 1: 10% ethanol, 10% cremophor, 80% D5W (dextrose 5%); vehicle for all other compounds (including SB-743921): 8% DMSO, 2% Tween 80, distilled water (pH 5). All treatments are given intraperitoneally. Vehicle control mice (group 1) are treated with 10 mL/kg vehicle on days 0, 3, 6, 8, 10, 13, 20, 22, 24, 29, 31, 34, 36, 38, 48, 51, 55, 58, 62, 65, and 69[3]. |
References: [1]. Jeffrey R. Jackson, et al. A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer. First AACR International Conference on Molecular Diagnostics in Cancer Therapeutic Development, Sep 12-15, 2006. | |
| Cas No. | 940929-33-9 | SDF | |
| Chemical Name | N-(3-aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxochromen-2-yl)-2-methylpropyl]-4-methylbenzamide;hydrochloride | ||
| Canonical SMILES | CC1=CC=C(C=C1)C(=O)N(CCCN)C(C2=C(C(=O)C3=C(O2)C=C(C=C3)Cl)CC4=CC=CC=C4)C(C)C.Cl | ||
| Formula | C31H34Cl2N2O3 | M.Wt | 553.53 |
| Solubility | ≥ 55.4mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8066 mL | 9.0329 mL | 18.0659 mL |
| 5 mM | 0.3613 mL | 1.8066 mL | 3.6132 mL |
| 10 mM | 0.1807 mL | 0.9033 mL | 1.8066 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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